Drug and route | Brand name | Injection interval | Available dose strengths | Maximum dose | Initiation and conversion from oral therapy | Injection site and technique | Solubilization and vehicle |
Second-generation | |||||||
Aripiprazole (IM) | Abilify Maintena | 4 weeks | 300 mg 400 mg | 400 mg every 4 weeks | Single injection start: Overlap with oral aripiprazole (or other oral antipsychotic) for 14 days after first LAI dose. Initiate LAI with 400 mg every 4 weeks. or Alternative double injection start:[1] Two injections of 400 mg (at different sites) administered concurrently with a single dose of 20 mg oral aripiprazole, followed by 400 mg IM every 4 weeks*. | Deltoid or gluteal; standard IM injection | Low solubility particles in aqueous suspension |
Abilify Asimtufii | 8 weeks | 720 mg 960 mg | 960 mg every 8 weeks | Overlap with oral aripiprazole (or other oral antipsychotic) for 14 days after first LAI dose. Initiate LAI with 960 mg every 8 weeks. If switching from 4-week aripiprazole LAI (Abilify Maintena), administer first dose of 960 mg in place of next scheduled injection; do not overlap with oral treatment. | Gluteal; standard IM injection | Low solubility particles in aqueous suspension | |
Aripiprazole lauroxil (IM) | Aristada | 4, 6, or 8 weeks (dose dependent) | 441 mg 662 mg 882 mg 1064 mg | 882 mg every 4 weeks | 21-day oral overlap start: Overlap with oral aripiprazole for 21 days after the first LAI dose; starting LAI dose is based on oral aripiprazole dose as follows:
or 1-day oral overlap start (using Aristada Initio): Single dose of 30 mg oral aripiprazole plus a one-time 675 mg Aristada Initio loading dose; may be given on same day or up to 10 days prior to first maintenance aripiprazole lauroxil LAI dose (based on oral dose using conversion above) with no additional oral overlap. | Gluteal (441 mg dose may also be administered in the deltoid); standard IM injection | Low solubility particles in aqueous suspension |
Aristada Initio nanocrystal dispersion (for optional loading dose or re-initiation after missed doses only) | Once | 675 mg | N/A | Deltoid or gluteal; standard IM injection | Nanoparticles in aqueous suspension | ||
Olanzapine pamoate (IM)¶ | Zyprexa Relprevv | 2 or 4 weeks (dose dependent) | 210 mg 300 mg 405 mg | 300 mg every 2 weeks or 405 mg every 4 weeks | No oral overlap required; starting LAI dose is based on stable dose of oral olanzapine as follows:
| Gluteal; standard IM injection | Nanoparticles in aqueous suspension |
Paliperidone palmitate (IM)Δ | Invega Sustenna; Erzofri (4-week) | 4 weeks | 39 mg 78 mg 117 mg 156 mg 234 mg 351 mg (Erzofri loading dose only) | 234 mg every 4 weeks | No oral overlap required. Loading dose:
Maintenance dose: Initiate 4 weeks after loading dose is complete (5 weeks after first Invega Sustenna dose); dose is based on stable dose of oral extended-release paliperidone as follows:
| Deltoid (load or maintenance) or gluteal (maintenance only); standard IM injection | Nanoparticles (Invega Sustenna) or low solubility particles (Erzofri) in aqueous suspension |
Invega Trinza (12-week) | 12 weeks (3 months) | 273 mg 410 mg 546 mg 819 mg | 819 mg every 12 weeks | Use only after adequate treatment and dose has been established with paliperidone palmitate 4-week LAI suspension for ≥4 months; the last two 4-week injection cycles should be the same dose before initiation. Dose is based on last dose of paliperidone palmitate 4-week LAI and is administered at the time the next dose is due as follows:
| Deltoid or gluteal; standard IM injection | Nanoparticles in aqueous suspension | |
Invega Hafyera (6-month) | 6 months | 1092 mg 1560 mg | 1560 mg every 6 months | Use only after adequate treatment and dose has been established with paliperidone palmitate 4-week LAI for a minimum of 4 months (the last two 4-week injection cycles should be the same dose before initiating) or paliperidone palmitate 12-week LAI for 1 cycle (3 months). Dose is based on last dose of paliperidone 4- or 12-week LAI and is administered at the time the next dose is due as follows:
| Gluteal; standard IM injection | Low solubility particles in aqueous suspension | |
Risperidone (IM) | Risperdal consta; Rykindo◊ | 2 weeks | 12.5 mg 25 mg 37.5 mg 50 mg | 50 mg every 2 weeks | Overlap with full-dose oral treatment for first 3 weeks (Risperdal Consta) or first week (Rykindo); starting LAI dose is based on stable dose of oral risperidone as follows:
| Deltoid (Risperdal Consta only) or gluteal; standard IM injection | Microsphere matrix in aqueous suspension |
Risvan | 4 weeks | 75 mg 100 mg | 100 mg every 4 weeks | No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
| Deltoid or gluteal; standard IM injection | Suspended in copolymer solution | |
Risperidone (SUBQ) | Perseris | 4 weeks | 90 mg 120 mg | 120 mg every 4 weeks | No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
| Abdomen or back of the upper arm; SUBQ injection | Suspended in polymer solution |
Uzedy | 4 or 8 weeks (dose dependent) | 50 mg 75 mg 100 mg 125 mg 150 mg 200 mg 250 mg | 125 mg every 4 weeks or 250 mg every 8 weeks | No oral overlap required; starting LAI dose is based on stable dose of oral risperidone as follows:
| Abdomen or back of the upper arm; SUBQ injection | Suspended in copolymer solution | |
First-generation | |||||||
Flupentixol decanoate (IM)§ | Fluanxol Depot | Variable; typically 2 to 4 weeks | 20 mg/mL 100 mg/mL | 100 mg every 2 weeks | Overlap with oral treatment at descending doses for first week; initiate LAI at 4 times daily oral dose every 2 weeks or 8 times daily oral dose every 4 weeks. Usual dose range: 10 to 50 mg. | Gluteal or lateral thigh¥; Z-track IM injection | Ester in medium chain triglycerides or coconut oil |
Fluphenazine decanoate (IM)‡ | Prolixin decanoate | Variable; typically 2 to 4 weeks | 25 mg/mL | 100 mg every 2 weeks | Initial 6.25 to 25 mg or use the following conversion from oral fluphenazine:
Overlap with oral therapy at one-half daily oral dose following the first injection; may discontinue oral therapy at time of the second injection. Usual dose range: 6.25 to 100 mg. | Gluteal†; Z-track IM | Ester in sesame seed oil |
Haloperidol decanoate (IM) | Haldol decanoate | 3 or 4 weeks | 50 mg/mL 100 mg/mL | 450 mg every 4 weeks | The first haloperidol decanoate LAI dose should not exceed 100 mg; if larger doses are required based on oral dose conversion, administer the first dose in two separate injections with 100 mg administered on day 1 and the remainder administered in 3 to 7 days. If the total dose ≥400 mg, it is given in a series of 3 injections. Subsequent doses may be administered as a single injection. Options for initiation include the following:
Usual dose range: 50 to 200 mg (10 to 15 times previous oral dose). | Gluteal†; Z-track IM injection | Ester in sesame seed oil |
Zuclopenthixol decanoate (IM)§ | Clopixol Depot | 2 to 4 weeks | 200 mg/mL (variable; usual dose range: 100 to 400 mg) | 600 mg every 2 weeks | Oral overlap with tapering may be considered during transition; starting LAI dose is based on stable dose of oral zuclopenthixol as follows:
| Gluteal or lateral thigh¥; Z-track IM injection | Ester in low viscosity 20% vegetable oil |
CYP: cytochrome P450; IM: intramuscular; LAI: long-acting injectable (also known as "depot" injection); SUBQ: subcutaneous.
* Aripiprazole double injection (ie, two IM doses of 400 mg each at separate sites) is off-label in the United States but is approved in other countries.[1]
¶ A lower starting dose of 150 mg every 4 weeks may be used in patients who are debilitated, at risk for orthostatic hypotension, or may metabolize more slowly (eg, nonsmoking, female, ≥65 years of age).
Δ Paliperidone LAI dosing in the United States labeling is based on paliperidone palmitate; dosing in some other areas (eg, Canada, United Kingdom, European Union) is based on paliperidone base (paliperidone palmitate 1 mg is equivalent to paliperidone base approximately 0.64 mg); refer to local product labeling.
◊ Rykindo is not a generic equivalent to Risperdal Consta; it has a more rapid onset. If switching from Risperdal Consta to Rykindo, initiate at same dose starting 4 weeks after the last injection; do not overlap with oral treatment.
§ Not available in the United States. Product details are from Health Canada product monographs.
¥ Lateral thigh administration is off-label in Canada, but is approved in other countries.
‡ Although SUBQ administration is described in the United States label, UpToDate contributors avoid SUBQ use. The required injection volumes (eg, >1.5 mL for doses >37.5 mg) may not be well tolerated.
† Alternatively, fluphenazine and haloperidol LAI may be given in the deltoid based upon clinical experience. For deltoid administration, use of a 23-gauge, 1-inch needle is appropriate for most adults; volume per injection is typically limited to 1 mL at this site. Deltoid administration is off-label and published clinical data are unavailable.
Data from UpToDate Lexidrug. More information available at https://online.lexi.com/.
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